|(R)-2-((6-(3-氨基哌啶-1-基)-3-甲基-2,4-二氧代-3,4-二氢嘧啶-1(2H)-基)甲基)苯甲腈苯甲酸盐|CsnPharm

CAS No.: 850649-62-6

苯甲酸阿格列汀 Catalog No. CSN12318

Synonyms: SYR 322;SYR-322 Benzoate;Alogliptin (benzoate salt)

Alogliptin benzoate is the benzoate salt form of alogliptin which is a selective inhibitor of DPP-4 with IC50 of 6.9 nM that exhibits greater selective than DPP-2, DPP-8 and DPP-9.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Dipeptidylpeptidase 4 (DPP4) belongs to the S9b gene family of postproline serine peptidases. It acts mostly as a secreted membrane protein, mediating the degradation and inactivation of glucagon-like peptide (GLP)-1 and gastric inhibitory protein (GIP). Alogliptin is a potent, selective inhibitor of the DPP-4 with IC_{50_{value of 2.63 nM in enzymatic assay. And it has nearly 1000-fold higher IC₅₀ for DPP8/9 inhibition than for DPP4 inhibition. In rats, dogs, and monkeys, the absolute oral bioavailability of alogliptin was 45%, 86%, and 72% to 88%, respectively. After a single oral dose of alogliptin, plasma DPP-4 inhibition was observed within 15 min and maximum inhibition was > 90% in rats, dogs, and monkeys; inhibition was sustained for 12 h in rats (43%) and dogs (65%) and 24 h in monkeys (> 80%). In Zucker fa/fa rats, a single dose of alogliptin (0.3, 1, 3, and 10 mg/kg) inhibited plasma DPP-4 (91% to 100% at 2 h and 20% to 66% at 24 h), increased plasma concentration of GLP-1 and early-phase insulin secretion and reduced blood glucose excursion after oral glucose challenge.}}
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02798172	Diabetes Mellitus, Type 2	Not Applicable	Completed	-	-
NCT01990300	-	-	Completed	-	-
NCT03499704	Diabetes Mellitus, Type 2	Phase 4	Not yet recruiting	December 31, 2020	-

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参考文献

[1] Rendell M, Drincic A, et al. Alogliptin benzoate for the treatment of type 2 diabetes. Expert Opin Pharmacother. 2012 Mar;13(4):553-63.
[2] Feng J, Zhang Z, et al. Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. J Med Chem. 2007 May 17;50(10):2297-300.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1668 mL
- 10.8339 mL
- 21.6679 mL
- 5 mM
- 0.4334 mL
- 2.1668 mL
- 4.3336 mL
- 10 mM
- 0.2167 mL
- 1.0834 mL
- 2.1668 mL

技术信息

CAS号

850649-62-6

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H27N5O4

运输

蓝冰

分子量

461.51

别名

SYR 322;SYR-322 Benzoate;Alogliptin (benzoate salt);Nesina;Kazano;Oseni;Alogliptin benzoate;苯甲酸阿格列汀

溶解度

DMSO	36.0 mg/mL (78.0 mM) warming
Water	10.0 mg/mL (21.7 mM) warming

动物实验配方

0.5% methylcellulose+water

30 mg/mL

suspension

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